Abstract: The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

Abstract: The present invention relates to conjugates including a residualizing linker, methods for their production, and uses thereof.

Abstract: The invention relates to compounds according to the general formula (I) or a pharmaceutically acceptable salt of an inorganic or organic acid, a hydrate, a stereoisomer or a solvate thereof, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 being selected independently of one another from hydrogen and alkoxy. The compounds of formula (I) as ligands are suitable for the production of radioactively labelled 68Ga, 64Cu, 67Ga, 111In or 99mTc complexes. The invention further relates to a method for producing the compounds of formula (I) and the radioactively labelled complexes and to the use of the radioactively labelled complexes in imaging methods, such as PET/CT, in particular of the liver.

Abstract: In some aspects, the present disclosure provides compounds of the formula: wherein the variables are defined herein. In some aspects, the present disclosure provides methods of preparing imaging agents, compositions thereof, and methods of imaging using said imaging agents or compositions thereof.

Abstract: The present invention is directed to glypican-3-specific peptide reagents, methods for detecting hepatocellular carcinoma cells using the peptide reagents, and methods for targeting hepatocellular carcinoma cells using the peptide reagents.

Abstract: The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

Abstract: A compound for radio metal complexation includes a chelator and one or more biological targeting vectors TV conjugated to said chelator, wherein the chelator has structure (A) or (B) or (C), based on 1,4-diazepine with groups R1, R2, R3, R4, X1, X2, X3. The compound is particularly suited for complexation of radio-isotopic metals, such as 66Ga(III), 67Ga(III) and 68Ga(III).

Abstract: The present invention relates to a process to prepare N,N?-di(2-hydroxybenzyl) ethylenediamine-N,N?-diacetic acid and salts thereof comprising a reaction between formaldehyde, ethylenediamine diacetic acid or a salt thereof and phenol at a pH of between 3 and 7 and a temperature below 60° C. wherein the reaction mixture contains 0.2 to 1.1 molar equivalents of alkali metalions on the molar amount of EDDA.

Abstract: A method for stabilization of potent alkanone-heterocyclic flavorants in dry powder form is provided. Coordination of alkanone-heterocyclic flavorants to transition metal salts results in the formation of stable crystalline complexes, which upon hydration release the free flavorant. Food and topping products containing the stabilized alkanone-heterocyclic flavorant are provided as are methods for stabilizing the alkanone-heterocyclic flavorant.

Abstract: A tetradentate organic ligand H3-MN-16Bn containing a long alkyl group, a precursor thereof, and a method for preparing the same are revealed. A precursor of H3-MN-16Bn, benzyl 16-bromohexadecanate, is obtained by esterification reaction of 16-bromohexadecanoic acid. Then bimolecular nucleophilic substitution reaction (SN2) of Benzyl 16-bromohexadecanate with nitrogen sulfide (N2S2) is carried out to get H3-MN-16Bn that is used as a standard hydrolysis metabolites of non-radioactive 185Re-complex compound.

Abstract: A method for stabilization of potent alkanone-heterocyclic flavorants in dry powder form is provided. Coordination of alkanone-heterocyclic flavorants to transition metal salts results in the formation of stable crystalline complexes, which upon hydration release the free flavorant. Food and topping products containing the stabilized alkanone-heterocyclic flavorant are provided as are methods for stabilizing the alkanone-heterocyclic flavorant.

Abstract: The present invention relates to manganese(II). The invention also relates to manganese(II) chelates attached to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).

Abstract: The present invention concerns radioactive rhodium complexes, their preparation methods, and their use for the radiolabelling of biomolecules, especially monoclonal antibodies.

Abstract: Described are bifunctional NOTA-based derivatives capable of conjugating with alginate and with metal ions, as well as NOTA-alginate conjugates which can be labeled with stable or radioactive metal ions. Also described are conjugation methods of the bifunctional NOTA-based linker with alginate, and methods of using radiometal-labeled NOTA-alginate conjugates or other radio-labeled alginate conjugates as imaging reagents.

Abstract: The invention relates to novel multi-modality probes for imaging, tracking and analyzing stem cells and related biological samples, and methods of preparation and use thereof. The molecular probes of the invention are constructed, for example, by utilizing (a) the high selectivity of long hydrocarbon chains for binding to plasma membranes of cells, (b) a near-infrared (NIR) dye for optical imaging, and (c) a radionuclide for PET or SPECT imaging. The in vitro and in vivo data of the optical and radiolabeled probes demonstrated their utility for detecting the presence of stem cells with multiple imaging modalities.

Abstract: The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: Pharmaceutical compositions may include a complex of a radionuclide and a compound of Formula I or Formula II.

Abstract: The present invention relates to copper, gallium and technetium coordinated thiosemicarbazone-pyridylhydrazine (substituted at the pyridine ring with a substituted benzothiazole or stilbene moiety) complexes and methods thereof. Such compounds possess utility in PET imaging and diagnosis of amyloid diseases.

Abstract: The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.

Abstract: The present invention relates to a 68Ga generator, wherein the 68Ge parent nuclide thereof is attached specifically to a support through a triethoxyphenyl group and continuously disintegrates to 68Ga, the triethoxyphenyl group being covalently bound to a support material through a linker.

Abstract: A radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same are revealed. The radiotracer precursor, DANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus DANI can be used to produce radiotracers stayed in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.

Abstract: Tracers that can be used for PET or SPECT imaging of the distribution of Pgp are disclosed. The tracers are metalloprobes that can comprise a radioactive metal ion such as 67Ga or 68Ga. Methods of synthesizing the tracers, and methods of imaging heart and other tissues are also disclosed. The tracers can be used to obtain high signal-to-background ratios for imaging tissues in vivo such as heart or tumor tissue. In various embodiments, disclosed tracers can exhibit, a) enhanced first pass extraction into heart tissue compared to presently available probes, b) linearity with true blood flow, c) enhanced detection of myocardial viability compared to presently available probes, d) reduced liver retention compared to presently available probes, and e) more efficient clearance from non-cardiac and adjoining tissues compared to presently available probes.

Abstract: Novel radiopharmaceuticals that are useful in diagnostic imaging and therapeutic treatment of disease characterized by over expression of CA-IX comprise a complex that contains a sulfonamide moiety which is capable of binding the active catalytic site of CA-IX, and a radionuclide adapted for radioimaging and/or radiotherapy:

Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecu le, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

Abstract: Compounds as defined herein are provided which are useful in (1) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable diluent; and (3) methods for imaging prostate cancer cells.

Abstract: The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.

Abstract: The invention provides D02S derivatives conjugated to monosaccharide ligands directly or through a linker and optionally chelated to a metal, wherein the D02S derivatives having the following structure: wherein R1?, R2? are each independently —OH or —O-alkyl; R1 is a hydrogen, a linker, or a ligand; R3 is a linker and/or a ligand; and n is an integer from 1 to 10; the linker is an amino acid, a peptide, an amino alcohol, a polyethylylene glycol, an alkyl, an alkenyl, an alkynyl, an azide, an aromatic compound, a carboxylic acid, or an ester, the alkyl, alkenyl, or alkynyl is optionally substituted with an alkyl, a halogen, a nitro group, a hydroxyl group, an amino group, or a carboxyl group; the ligand is a GLUT1 targeting moiety.

Abstract: The present disclosure provides a novel class of macrocyclic compounds and their metal complexes formed with transition metal ion, lanthanide metal ions and other metal ions (e.g., Al, Ga, Y, In, Sn, Tl, Pb and Bi) and their applications in the fields of contrast agents, artificial nucleases, fluorescence probes, nuclear medicines and other biomedical applications in the therapeutics or diagnostics.

Abstract: The present invention relates to a 68Ga generator, wherein the 68Ge parent nuclide thereof is attached specifically to a support through a triethoxyphenyl group and continuously disintegrates to 68Ga, the triethoxyphenyl group being covalently bound to a support material through a linker.

Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.

Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.

Abstract: The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4)alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or a group of formula (?): —Y—Z—W—R11??(?) wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a —N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.

Abstract: The present application discloses 17? hydroxy steroid dehydrogenase (17? HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17? HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17? HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17? HSD1 and 17? HSD3 that have a spiro-morpholine substituent at C20.

Abstract: This invention includes agents and compositions having MRI, PET, CT, X-ray, SPECT or optical signals, and methods for their use in the determination of a target. In some cases, a MRI, PET, CT, X-ray, SPECT, optical or other signal produced by the agent or composition can be affected by the presence of the target. Examples of targets that can be determined by this invention include, but are not limited to zinc, copper, iron ions and other biological targets. Example of application for imaging in vivo includes the function of pancreas and other organs.

Abstract: The present invention provides radioactive arsenic complex useful in diagnostic and therapeutic applications and methods for forming those arsenic complexes.

Abstract: The present invention provides luminescent complexes between a lanthanide ion and an organic ligand which contains 1,2-hydroxypyridinone units. The complexes of the invention are stable in aqueous solutions and are useful as molecular probes, for example in medical diagnostics and bioanalytical assay systems. The invention also provides methods of using the complexes of the invention.

Abstract: A precursor used for labeling hepatocyte receptors and applied to radiotracers for imaging or pharmaceutical compositions for liver cancers is revealed. The precursor is a bifunctional compound. The bifunctional group includes a trisaccharide structure and a diamide dimercaptide (N2S2) ligand. The trisaccharide has high affinity to asialoglycoprotein receptors (ASGPR) on surfaces of hepatocytes while N2S2 ligand reacts with radioisotopes to form neutral complexes. Thus the precursor stays on surfaces of hepatocytes to provide radioisotope labeling or treatment effect of liver cancers.

Abstract: A dendrimer conjugate according to Formula (I), or its pharmaceutically acceptable salt, or solvate thereof: and complexes of Formula I conjugates with metals radionuclides of elements such as rhenium, technetium, yttrium, lutetium and others to provide a complex for imaging tissues or for the radiotherapeutic treatment of cancer tissue. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.

Abstract: The invention relates to a method and a kit for preparing a radiopharmaceutical, the method comprising the steps: elution of a 68Ge/68Ga-Generator using hydrochloric acid as an eluent for obtaining a generator eluate comprising 68Gallium, feeding the generator eluate through a cation exchange cartridge, which collects the 68Gallium, separating the used eluent, eluting the 68Gallium from the cation exchange cartridge using a solution comprising sodium chloride and hydrochloric acid and feeding the resulting eluate into an aqueous precursor mixture comprising at least a labelling precursor thereby forming a reaction solution.

Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

Abstract: The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.

Abstract: The present invention is directed to CA IX inhibitors that conform to Formula I where the substituents X, A, B, D, E, E? and G are as defined above. Also described are Pt, 64Cu, 186Re, 188Re and 99mTc metal complexes of Formula I compounds which find use as candidate agents for imaging tumors.

Abstract: The present invention discloses alpha particle emitting, radioactive constructs capable of killing large tumors (>1 mm in diameter), or other cells involved in human or animal diseases such as virus infected cells, autoimmune cells, or other pathological cells, including normal cells, that are targets for destruction, to achieve a therapeutic result. The alpha-emitting constructs have high specific activity.

Abstract: The present invention provides novel in vivo imaging agents useful for detecting the presence of mycobacteria using in vivo imaging methods. Also provided by the present invention is a precursor compound useful in the synthesis of the in vivo imaging agents of the invention, and a method to obtain the in vivo imaging agent of the invention using said precursor compound. Methods of in vivo imaging and diagnosis in which the in vivo imaging agent of the invention finds use are also provided.

Abstract: Described are bifunctional NOTA-based derivatives capable of conjugating with alginate and with metal ions, as well as NOTA-alginate conjugates which can be labeled with stable or radioactive metal ions. Also described are conjugation methods of the bifunctional NOTA-based linker with alginate, and methods of using radiometal-labeled NOTA-alginate conjugates or other radio-labeled alginate conjugates as imaging reagents.

Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: The invention also provides pharmaceutical compositions of a complex of a radionuclide and a Formula I compound or a Formula II compound and methods of using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The present invention involves a new synthesis route for the formation of lactylates. The method comprises reacting a dilactide with a compound comprising a hydroxy group. This reaction is preferably carried out in the presence of a cation or other source of alkalinity. Preferred compounds comprising a hydroxy group include any fatty acid and fatty acid alcohol (particularly C1-C26 fatty acid chains). Preferred cations include cations of Group I and II metals, with sodium, calcium, and potassium cations being particularly preferred. The inventive reactions proceed much more rapidly than prior art lactylate synthesis reactions, and can be used to form 1-, 2-, 3-, 4-, and 5-lactylates.